Tajuddeen Nasir, Swart Tarryn, Hoppe Heinrich C, van Heerden Fanie R
School of Chemistry and Physics, University of KwaZulu-Natal, Private Bag X01, Scottsville 3209, South Africa.
Department of Biochemistry & Microbiology, Rhodes University, Grahamstown 6140, South Africa.
Pharmaceuticals (Basel). 2022 Apr 13;15(4):470. doi: 10.3390/ph15040470.
is used in Zulu traditional medicine as an antimalarial remedy. A moderate antiplasmodial activity was previously reported for extracts of the plant against D10 . This study aimed to identify the phytochemicals responsible for the antiplasmodial activity of the leaf extract. The compounds were isolated by chromatography and their structures were determined using spectroscopic and spectrometric methods. The antiplasmodial activity was evaluated using a parasite lactate dehydrogenase assay and cytotoxicity was determined using a resazurin assay. The ethyl acetate fraction inhibited . with IC = 10.6 µg/mL and showed minimal cytotoxicity (98% cell viability at 33 µg/mL). The chromatographic purification of this fraction afforded sixteen compounds, including two new flavonoids. A 1:1 mixture of phytol and lupeol was also isolated from the hexane fraction. All the compounds were reported from for the first time. Among the isolated metabolites, methyl gallate displayed the best activity against (IC = 1.2 µg/mL), with a 68% viability of HeLa cells at 10 µg/mL. Therefore, methyl gallate was responsible for the antiplasmodial activity of the leaf extract and its presence in the leaf extract might account for the folkloric use of the plant as an antimalarial remedy.
在祖鲁传统医学中用作抗疟疾药物。此前有报道称该植物提取物对D10具有中等抗疟活性。本研究旨在鉴定叶提取物中具有抗疟活性的植物化学成分。通过色谱法分离化合物,并使用光谱和光谱测定方法确定其结构。使用寄生虫乳酸脱氢酶测定法评估抗疟活性,并使用刃天青测定法确定细胞毒性。乙酸乙酯馏分抑制……,IC50 = 10.6 µg/mL,且细胞毒性最小(在33 µg/mL时细胞活力为98%)。该馏分的色谱纯化得到了16种化合物,包括两种新的黄酮类化合物。还从己烷馏分中分离出了叶绿醇和羽扇豆醇的1:1混合物。所有化合物均为首次从……中报道。在分离出的代谢产物中,没食子酸甲酯对……表现出最佳活性(IC50 = 1.2 µg/mL),在10 µg/mL时HeLa细胞活力为68%。因此,没食子酸甲酯是该植物叶提取物抗疟活性的原因,其在叶提取物中的存在可能解释了该植物作为抗疟疾药物的民间用途。